1225037-39-7
Chemical Structure
Bimiralisib
Synonym(s): PQR309
- CAS No.: 1225037-39-7
- Formula:C17H20F3N7O2
- Molecular Weight:411.38
IUPAC Name: 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine
InChIKey: ADGGYDAFIHSYFI-UHFFFAOYSA-N
SMILES: NC1=NC=C(C2=NC(N3CCOCC3)=NC(N4CCOCC4)=N2)C(C(F)(F)F)=C1
Biological Activity: Bimiralisib (PQR309) is an orally active, blood-brain barrier-penetrant PI3K/mTOR inhibitor with in vitro antiproliferative activity and in vivo antitumor activity. Bimiralisib induces G1 cell cycle arrest, apoptosis and cell death in cancer cells, while inhibiting cancer cell proliferation, migration, invasion, colony formation and spheroid generation. Bimiralisib upregulates the expression of E2F4. The combination of Bimiralisib with venetoclax enhances therapeutic efficacy in acute myeloid leukemia models. Bimiralisib can be used in cancer-related research[1][2][3][4].
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Bimiralisib | 98.62% | Bimiralisib (PQR309) is an orally active, blood-brain barrier-penetrant PI3K/mTOR inhibitor with in vitro antiproliferative activity and in vivo antitumor activity. Bimiralisib induces G1 cell cycle arrest, apoptosis and cell death in cancer cells, while inhibiting cancer cell proliferation, migration, invasion, colony formation and spheroid generation. Bimiralisib upregulates the expression of E2F4. The combination of Bimiralisib with venetoclax enhances therapeutic efficacy in acute myeloid leukemia models. Bimiralisib can be used in cancer-related research. | ||||||||||||||||||||
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References
- [1]. Wu X, et al. Recent Advances in Dual PI3K/mTOR Inhibitors for Tumour Treatment. Frontiers in pharmacology. 2022;13:875372.
- [2]. Seipel K, et al. Rationale for Combining the BCL2 Inhibitor Venetoclax with the PI3K Inhibitor Bimiralisib in the Treatment of IDH2- and FLT3-Mutated Acute Myeloid Leukemia. International journal of molecular sciences. 2022 Oct 20;23(20):12587. [Content Brief]
- [3]. Noh YJ, et al. Bimiralisib suppresses proliferation and migration of gastric cancer cells PI3K/mTOR pathway inhibition. The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology. 2026 Jul 08. [Content Brief]
- [4]. Beaufils F, et al. 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. J Med Chem. 2017 Sep 14;60(17):7524-7538.
